An evaluation of tamoxifen as a partial agonist by classical receptor theory — An explanation of the dual action of tamoxifen

Abstract

Tamoxifen is known to have both agonist and antagonist properties. Classical receptor theory predicts that given the relative concentrations of a partial agonist and full agonist acting on the same receptor, the partial agonist may reduce the effect of the full agonist. The immature rat uterine model is an excellent system to evaluate the interactions of estradiol and tamoxifen by application of receptor theory. Using this model, tamoxifen demonstrates both additive and antagonistic effects to estradiol in the fashion predicted by theory. The effects of tamoxifen are additive at low doses of estradiol and antagonistic over higher estradiol doses. It is possible that the dualism of agonism and antagonism seen in other target organs and species is a function of these basic characteristics of a partial agonist.